2. JAK/STAT Signaling Stem Cell/Wnt
  3. STAT
  4. ZDZ-553

ZDZ-553 是一种具有口服活性的 STAT1 抑制剂，其 IC50 值为 0.87 μM。ZDZ-553 可调控 STAT1 信号通路，从而影响下游脂质代谢及炎症通路。ZDZ-553 可减轻非酒精性脂肪性肝炎 (NASH) 小鼠模型中的肝脂肪变性。ZDZ-553 可降低 NASH 小鼠模型中的炎症反应。ZDZ-553 具有明确的安全性特征。ZDZ-553 可用于非酒精性脂肪性肝炎的相关研究。

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ZDZ-553

ZDZ-553 Chemical Structure

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ZDZ-553 相关抗体

Top Publications Citing Use of Products

查看 STAT 亚型特异性产品:

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STAT3 STAT5 STAT6 STAT1

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

ZDZ-553 is an orally active STAT1 inhibitor with an IC50 value of 0.87 μM. ZDZ-553 modulates STAT1 signaling to affect downstream lipid metabolism and inflammatory pathways. ZDZ-553 attenuates hepatic steatosis in NASH mouse models. ZDZ-553 reduces inflammatory responses in NASH mouse models. ZDZ-553 exhibits a defined safety profile. ZDZ-553 can be used for the research of nonalcoholic steatohepatitis[1].

IC50 & Target[1]

STAT1

0.87 μM (IC50, 文献未验证pan或者selective)

体外研究
(In Vitro)

ZDZ-553 (24 h) 可强效抑制稳定型 293T-STAT1/GAS-Luc 细胞中的 STAT1 活性，其 IC50 为 0.87 μM，且在最高达 200 μM 的浓度下无细胞毒性[1]。
ZDZ-553 (0.052 μM; 0, 30, 60, 120 min) 在人、小鼠和大鼠肝微粒体中具有优异的代谢稳定性，所有物种的 T1/2 >120 min[1]。
ZDZ-553 (以 200 μM 为起始浓度进行系列 2 倍稀释；24 h) 浓度高达 200 μM 时对 HepG2 细胞无细胞毒性[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

ZDZ-553 相关抗体:

Cell Cytotoxicity Assay[1]

Cell Line: HepG2 cells
Concentration: 0-200 μM (serial 2-fold dilutions starting at 200 μM)
Incubation Time: 24 h
Result: Showed no cytotoxicity after 24 h of exposure, with no decrease in cell viability even at the highest tested concentration of 200 μM.
药代动力学
(Parmacokinetics)
Species Dose Route AUC0-inf Cmax T1/2 MRT0-inf Tmax F
Rat[1] 30 mg/kg i.v. 69,512 ng·h/mL 2467 ng/mL 16.63 h 24.3 h / /
Rat[1] 30 mg/kg p.o. 12,599 ng·h/mL 819 ng/mL 12.18 h 18.8 h 1.13 h 18.1 %
体内研究
(In Vivo)

ZDZ-553 (30-60 mg/kg；灌胃；每日；4 周) 以 30 和 60 mg/kg 剂量经口给药 4 周后，可呈剂量依赖性改善 HF-CDAA 诱导的 NASH 小鼠的肝脂肪变性、肝损伤及炎症反应，且 60 mg/kg 剂量的疗效优于 30 mg/kg 剂量及阳性对照药 Dios[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL/6J (male, 7−8 weeks old, 20-23 g, HF-CDAA diet-induced)[1]
Dosage: 30 mg/kg; 60 mg/kg
Administration: p.o.; daily; 4 weeks
Result: Reduced hepatic triglyceride (TG) and total cholesterol (TC) levels, reduced serum ALT and AST levels; reduced mRNA expression of hepatic acetyl-CoA carboxylase (ACC), fatty acid synthase (FASN), FATP-1, IL-6, IL-1β, TNF-α, and CXCL10; decreased NAFLD Activity Score (NAS) compared to vehicle controls; reduced hepatocellular ballooning (H&E staining) and reduced size/quantity of lipid droplets (Oil Red O staining) at 30 mg/kg.
Produced greater dose-dependent reductions in hepatic TG, TC, serum AST, and mRNA expression of ACC, FASN, FATP-1, IL-6, IL-1β, TNF-α, and CXCL10 compared to the 30 mg/kg dose; resulted in a larger decrease in NAS compared to the 30 mg/kg dose; showed more pronounced improvements in hepatocellular ballooning and lipid droplet accumulation (histological staining) compared to the 30 mg/kg dose at 60 mg/kg.
Showed more significant reductions in hepatic TG, TC, serum AST, and inflammatory cytokine mRNA expression than the positive control Dios at 60 mg/kg at both doses.
分子量

404.26

Formula

C18H10F6O4
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

ZDZ-553 相关分类

  • 摩尔计算器

  • 稀释计算器

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

ZDZ-553ZDZ553ZDZ 553STATrat liver microsomeslipid metabolismNASH mouse modelsmouse liver microsomeshuman liver microsomesSTAT1hepatic steatosisHepG2 cellsinflammatory pathways293T-STAT1/GAS-Luc cellsInhibitorinhibitorinhibit

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